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Assay Detail

CHEMBL5161260

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of ROCK2 (unknown origin)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Rho-associated protein kinase 2 (CHEMBL2973)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain.
Luo G, Chen L, Kostich WA, Hamman B, Allen J, Easton A, Bourin C, Gulianello M, Lippy J, Nara S, Pattipati SN, Dandapani K, Dokania M, Vattikundala P, Sharma V, Elavazhagan S, Verma MK, Lal Das M, Wagh S, Balakrishnan A, Johnson BM, Santone KS, Thalody G, Denton R, Saminathan H, Holenarsipur VK, Kumar A, Rao A, Putlur SP, Sarvasiddhi SK, Shankar G, Louis JV, Ramarao M, Conway CM, Li YW, Pieschl R, Tian Y, Hong Y, Bristow L, Albright CF, Bronson JJ, Macor JE, Dzierba CD.
J Med Chem (2022) 65 : 4534 -4564
PubMed 35261239 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.15 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5202142 1 6.85
CHEMBL5195653 1 6.11
CHEMBL5185000 1 5.96
CHEMBL5188433 1 5.96
CHEMBL5184381 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5202142 IC50 = 140.0 nM 6.85
CHEMBL5195653 IC50 = 780.0 nM 6.11
CHEMBL5185000 IC50 = 1100.0 nM 5.96
CHEMBL5188433 IC50 = 1100.0 nM 5.96
CHEMBL5184381 IC50 = 1300.0 nM 5.89